NSC697923

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSC697923 (NSC 697923) 是一种小分子，可特异性抑制泛素结合 (E2) 酶 Ubc13 (UBE2N)-Uev1A 的活性。

NSC697923 (NSC 697923) is a small molecule that specifically inhibits the activity of the ubiquitin-conjugating (E2) enzyme Ubc13 (UBE2N)-Uev1A; NSC697923 impedes the formation of the Ubc13 and ubiquitin thioester conjugate and suppresses constitutive NF-κB activity in ABC-DLBCL cells, inhibits NF-κB activation induced by PMA, but not by TNFα; specifically inhibits Ubc13-mediated polyubiquitin chain synthesis in vitro, does not inhibits UbcH5c-mediated polyubiquitin chain formation; inhibits the proliferation and survival of ABC-DLBCL cells and GCB-DLBCL cells.

Cell Viability Assay Cell Line:Three MYCN-amplified cell lines: IMR32, NGP, NB19 and three MYCN-non-amplified cell lines: CHLA-255, SK-N-AS, and SH-SY5Y Concentration:0-5 μM Incubation Time:24 hours Result:Significantly reduced NB cells viability in a dose-dependent manner. Also induced cell death in the p53 non-functional cell line SK-N-AS and p53 partially functional cell line NB-19.Western Blot Analysis Cell Line:p53 wild-type SH-SY5Y and IMR32 cells Concentration:3?μM Incubation Time:2 hours Result:Induced expression of p53-targeted gene p21 as well as the cleavage of caspase 3 in two p53 wild-type cell lines SH-SY5Y and IMR32.

Animal Model:5- to 6-week-old female athymic Ncr nude mice (orthotopic mouse model of NB; SH-SY5Y and NGP xenografts) Dosage:5?mg/kg Administration:I.p.; daily for 10 days Result:Significant tumor regression in both SH-SY5Y and NGP xenografts.

NSC 697923

Proteasome/Ubiquitin

E2

E2

Other Indications

——

343351-67-7

267.255

C11H9NO5S

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (748.33 mM)

O=[N+](C1=CC=C(S(=O)(C2=CC=C(C)C=C2)=O)O1)[O-]

2-nitro-5-tosylfuran

(-20℃)

With Ice Pack

≥ 2 years